pH敏感O-羧甲基壳聚糖自组装纳米粒的制备及表征  

Preparation and characterization of self-assembled pH-sensitive O-carbohydrate chitosan nanoparticles

作　　者：覃志忠[1] 张凤宝[1] 张国亮[1] 宋秀娟[2] 

机构地区：[1]天津大学化工学院,天津300072 [2]沧州师范专科学校,河北沧州061600

出　　处：《现代化工》2009年第4期53-56,共4页Modern Chemical Industry

摘　　要：用5β-胆烷酸(5β-CHA)对O-羧甲基壳聚糖(OCMC)进行疏水改性,接枝磺胺地托辛(SDM)以增强其pH敏感性,在pH=9的磷酸盐缓冲溶液中制备了对肿瘤组织具有靶向潜力的自组装纳米粒子。所得纳米粒粒径在100nm左右,且随5β-CHA接枝量的增加5β-CHA/OCMC纳米粒的粒径减小。自组装纳米粒有较低的临界聚集浓度(10-2mg/mL),在pH=7.4(人体正常pH)的水溶液中表现出高度稳定性。而当溶液的pH<6.8(肿瘤组织pH)时,接枝SDM的纳米粒子会迅速聚集,粒径剧增,且随SDM接枝量的增加pH敏感性增强。A novel cancer-targeting drug delivery system is synthesized by self-aggregating of O-carbohydrate chitosan （OCMC） which is hydrophobieally modified by 5β-cholanic acid（5β-CHA） and grafted with sulfonamide（SDM）to enhance its pH sensitivity. The self-aggregates are successfully obtained in pbosphate buffer solution （PBS） at pH 9.0. The average diameter of the particles is approximately and uniformly 100nm, and the particle size of 5β-CHA/OCMC decreases with increasing the degree of of stitution of 5β-CHA due to the forming of a fighter hydrophobic core. With low critical aggTegate concentration （CAC） of about 10-2mg/mL, the self-aggregated particles show great stability at pH 7.4, which equals the nomud pH value of human body fluid. But belhiw pH 6.8, which is close to the tumor＇s pH value, the particles bearing SDM show good pH sensitivity by shrinking and aggregating. The pH sensitivity, can be enhanced with the increase of substitution degree of SDM.

关 键 词：自组装纳米粒 O-羧甲基壳聚糖 PH敏感性 5β-胆烷酸 磺胺地托辛 

分 类 号：R914[医药卫生—药物化学]